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Bioorg. Med. Chem. Lett. · Dec 2009
2-Aminopyrazolo[1,5-a]pyrimidines as potent and selective inhibitors of JAK2.
- Mark W Ledeboer, Albert C Pierce, John P Duffy, Huai Gao, David Messersmith, Francesco G Salituro, Suganthini Nanthakumar, Jon Come, Harmon J Zuccola, Lora Swenson, Dina Shlyakter, Sudipta Mahajan, Thomas Hoock, Bin Fan, Wan-Jung Tsai, Elaine Kolaczkowski, Scott Carrier, James K Hogan, Richard Zessis, S Pazhanisamy, and Youssef L Bennani.
- Vertex Pharmaceuticals Inc, Cambridge, MA 02139-4242, United States. mark_ledeboer@vrtx.com
- Bioorg. Med. Chem. Lett. 2009 Dec 1; 19 (23): 6529-33.
AbstractConstitutive activation of the EPO/JAK2 signaling cascade has recently been implicated in a variety of myeloproliferative disorders including polycythemia vera, essential thrombocythemia and myelofibrosis. In an effort to uncover therapeutic potential of blocking the EPO/JAK2 signaling cascade, we sought to discover selective inhibitors that block the kinase activity of JAK2. Herein, we describe the discovery and structure based optimization of a novel series of 2-amino-pyrazolo[1,5-a]pyrimidines that exhibit potent inhibition of JAK2.
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